Based on the well known biological versatility of the imidazoline nucleus, we prepared the novel derivatives 3a-k inspired by 2-BFI scaffold to assess imidazoline molecules as D(2)-like dopamine receptor ligands. Conservative chemical modifications of the lead structure, such as the introduction of an hydroxy group in the aromatic ring alone or associated with N-benzyl substitution, provided partial (3f) or nearly full (3e and 3h) agonists, all endowed with D(2)-like potency comparable to that of dopamine.

Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI

COSTA, BARBARA;MARTINI, CLAUDIA;
2010

Abstract

Based on the well known biological versatility of the imidazoline nucleus, we prepared the novel derivatives 3a-k inspired by 2-BFI scaffold to assess imidazoline molecules as D(2)-like dopamine receptor ligands. Conservative chemical modifications of the lead structure, such as the introduction of an hydroxy group in the aromatic ring alone or associated with N-benzyl substitution, provided partial (3f) or nearly full (3e and 3h) agonists, all endowed with D(2)-like potency comparable to that of dopamine.
Giorgioni, G; Ambrosini, D; Vesprini, C; Hudson, A; Nasuti, C; DI STEFANO, A; Sozio, P; Ciampi, O; Costa, Barbara; Martini, Claudia; Carrieri, A; Carbonara, G; Enzensperger, C; Pigini, M.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/204584
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